JP2019043862A - Composition for mitigating fatigue feeling and improving stiffness - Google Patents

Abstract

To provide a composition and an agent useful for mitigating a fatigue feeling and improving stiffness.SOLUTION: The present invention provides a composition for mitigating a fatigue feeling and improving stiffness, containing a quercetin glycoside as an active ingredient.SELECTED DRAWING: Figure 1

Description

  The present invention relates to a composition for alleviating fatigue feeling or stiffness, a fatigue sensation alleviating agent and a stiffness improvement agent.

  The stiffness of the neck, shoulders and lower back is that the muscles become hard and that part feels heavy, which leads to a feeling of fatigue. A sense of fatigue is a major social problem because it causes a decline in activity and physical activity. In particular, office workers who frequently work in VDT (Visual Display Terminals) work with the same posture for a long time, and feel a strong sense of fatigue in their neck, shoulders and waist, leading to a decrease in work efficiency.

  The causes of stiffness vary, but the main cause is, for example, (1) fatigue of the eyes due to VDT work etc. As a result, the sympathetic nerve becomes excited and the blood vessels contract and blood circulation gets worse. (2) As a result of tension of the muscle by taking the same posture or unreasonable posture for a long time, the circulation of the blood becomes worse, (3) the sympathetic nerve becomes superior by mental tension, and the blood vessels in the muscle become Although it does shrink and does not use muscle, circulation worsens and waste products accumulate in muscle.

  Methods for eliminating fatigue and stiffness include needle and eyebrow method, blood flow improvement by massage or heat, etc., but many of them can not be easily performed at home or away from home. In addition, medicated bath agents and bath agent compositions (Patent Documents 1 and 2) are effective in improving fatigue and stiffness, but improve symptoms such as neck, shoulder, and waist stiffness that occur suddenly. It can not be said that it is effective.

  The application of a moistening agent (patent document 3) containing a blood circulation promoting agent is effective for the improvement of the feeling of fatigue or stiffness. However, the current situation is that use is not preferred because the peculiar odor of the poultice is muffled, and prolonged use causes irritation and irritation to the skin and the like.

  In addition, as a composition to be ingested in the form of pharmaceuticals and foods, Patent Document 4 discloses a blood flow improving action comprising cassis concentrate and at least one selected from the group consisting of amino acids and organic acids. A composition is disclosed. Further, Patent Document 5 discloses a vasodilator comprising a berry fruit and an organic acid component as active ingredients. However, there is a problem that the stability of anthocyanins in cassis and berry fruits is poor and it is difficult to use them in foods.

  Therefore, there is a demand for products that are expected to improve the quality of life (QOL), such as foods and pharmaceuticals that are effective for reducing fatigue and improving stiffness.

Japanese Patent Application Laid-Open No. 09-025226 Japanese Patent Application Laid-Open No. 11-158058 Japanese Patent Application Laid-Open No. 2000-07215 JP 2004-262878 A WO 2010/092941

  An object of the present invention is to provide a composition and an agent that are effective in reducing fatigue or improving stiffness.

  The present inventors have found that quercetin glycosides have the effect of improving stiffness of the neck, shoulders and hips, and completed the present invention.

That is, the present invention provides the following inventions.
[1] A composition for relieving fatigue or improving stiffness comprising quercetin glycoside as an active ingredient.
[2] The composition for relieving fatigue or for improving stiffness according to [1], wherein the quercetin glycoside is α-glucosylrutin.
[3] The composition for alleviating fatigue or for improving stiffness according to [2], wherein the α-glucosylrutin is α-monoglucosylrutin.
[4] A fatigue sensation reducing agent containing quercetin glycoside as an active ingredient.
[5] A set improving agent containing quercetin glycoside as an active ingredient.
[6] The fatigue sensation reducing agent according to [4], wherein the quercetin glycoside is α-glucosylrutin.
[7] The setting improving agent according to [5], wherein the quercetin glycoside is α-glucosylrutin.
[8] The fatigue sensation reducing agent according to [6], wherein the α-glucosylrutin is α-monoglucosylrutin.
[9] The stiffness improving agent according to [7], wherein the α-glucosylrutin is α-monoglucosylrutin.

  The compositions and agents of the present invention exert excellent stiffness-improving action in a single dose and in a short time to reduce fatigue and are useful for maintenance and promotion of physical and mental health.

FIG. 1A is a diagram showing that quercetin glycosides have the effect of improving neck and shoulder stiffness. FIG. 1B is also a view showing that quercetin glycoside has an effect of improving stiffness of the lower back. FIG. 2 is a view showing that quercetin glycosides have a ciliary muscle relaxing action.

  The composition for alleviating fatigue feeling or stiffness improvement of the present invention (hereinafter also referred to as the composition of the present invention) and the fatigue sensation reducing agent and stiffness improvement agent of the present invention (hereinafter also referred to as the agent of the present invention) A glycoside is contained as an active ingredient.

  In the present invention, "quercetin glycoside" refers to a glycoside of quercetin which is a kind of polyphenol, and is represented by the following formula (I).

  In formula (I), (X) n represents a sugar chain, and n is an integer of 1 or more.

  Here, as the sugar constituting the sugar chain represented by X which is bonded to quercetin by glycosidic bond, for example, glucose, rhamnose, galactose, glucuronic acid and the like can be mentioned, and glucose and rhamnose are particularly preferable. Further, n is not particularly limited as long as it is 1 or more, but is preferably 1 to 16, and more preferably 1 to 8. When n is 2 or more, the X moiety may be composed of one type of sugar chain, or may be composed of a plurality of sugar chains.

  The quercetin glycosides include those obtained by treating existing quercetin glycosides with an enzyme or the like and transglycosylating. Specific examples of quercetin glycosides include rutin, glucosylrutin, quercitrin and isoquercitrin.

  In one aspect of the present invention, one compound included in quercetin glycoside may be used alone, or a plurality of compounds may be mixed and used. The origin of quercetin glycosides is not particularly limited. For example, as a plant containing a large amount of quercetin or quercetin glycosides, buckwheat, enju, queper, apple, tea, onion, grape, broccoli, moth berry, raspberry, cowberry, cranberry , Opuntia, leafy vegetables, citrus fruits and the like.

  In addition, quercetin glycosides are extracts obtained by increasing the concentration of quercetin glycosides by concentration and operation of purified sugar, for example, using a concentrate or purified product of quercetin glycoside-containing extracts be able to. A conventionally known method can be used as the concentration method or purification method.

  In one aspect of the present invention, it is preferable to use α-glucosylrutin as a quercetin glycoside. α-glucosylrutin is a compound contained as a main component in a product known as “enzyme-treated rutin” (sometimes referred to as “glycotransfer rutin”) and is represented by the following formula (II) The compound having the following structure, that is, a compound in which one or more (about 2 to 20) glucoses are bound to a glucose residue in a rutinose residue possessed by rutin by α1 → 4 bond.

  In the present specification, among α-glucosylrutin, one in which only one glucose is bound is referred to as “α-monoglucosylrutin”, and one in which two or more glucose are bound is referred to as “α-polyglucosylrutin”.

  That is, in the following formula (II), α-glucosylrutin is generally a compound in which n is 1 to 20, α-monoglucosylrutin is a compound in which n is 1 and α-polyglucosylrutin is generally n is a compound of 2 to 20;

  Even in the case of α-monoglucosylrutin, the action and effect of the composition or agent of the present invention and the general action and effect on α-glucosylrutin are exhibited without problems, and the molecular weight of α-monoglucosylrutin is α-polyglucosyl Since the molecular weight of rutin is smaller than that of rutin, the number of molecules per unit mass is larger for α-monoglucosylrutin, which is considered to be advantageous in terms of effects. Therefore, it is preferable that a part or all of α-glucosylrutin be α-monoglucosylrutin.

  Enzymatically-treated rutin is a rutin in the presence of an α-glucosyl sugar compound (cyclodextrin, partially degraded starch, etc.), a rutin glycosyltransferase (cyclodextrin glucanotransferase (CGTase, EC2.4.1.19), etc.) It is a product obtained by acting an enzyme having a function of adding glucose to (hereinafter also abbreviated as first enzyme-treated rutin).

  The first enzyme-treated rutin contains various α-glucosylrutins different in the number of bound glucose, ie, an aggregate consisting of α-monoglucosylrutin and other α-glucosylrutin, and rutin which is an unreacted substance Composition. If necessary, the first enzyme-treated rutin is purified using, for example, a porous synthetic adsorbent and a suitable eluate to remove sugar donors and other impurities and to further reduce the content of rutin, The first enzyme-treated rutin (a purified product of α-glucosylrutin) having an increased purity of α-glucosylrutin is obtained.

  Alternatively, the first enzyme-treated rutin is treated with an enzyme having a glucoamylase activity, such as glucoamylase (EC 3.2.1.3), which cleaves an alpha-1,4-glucosidic bond at a glucose unit, and a plurality of glucose are In the added α-glucosylrutin, the α-glucosyl rutin itself is α- by leaving only one glucose residue directly attached to the glucose residue (in the rutinose residue) and leaving the other glucose residue. An enzyme-treated rutin containing a large amount of monoglucosylrutin (hereinafter also abbreviated as a second enzyme-treated rutin) can be obtained. This enzyme treatment does not cleave the glucose residue in the rutinose residue directly linked to the quercetin backbone from the quercetin backbone.

  α-glucosylrutin is contained as a main component in, for example, trade name “αG rutin PS”, trade name “αG rutin P”, trade name “αG rutin H”, and the like manufactured by Toyo Seika Sho Co., Ltd. These goods are compositions containing 10 to 90% by weight of α-monoglucosylrutin.

  The composition comprises (i) preparing the above-described first enzyme-treated rutin, (ii) treating the first enzyme-treated rutin with an enzyme having glucoamylase activity, and almost all α-glucosylrutin as α-monoglucosyl It can be manufactured by the procedure of converting it into rutin.

  The content of quercetin glycoside which is an active ingredient in the composition or agent of the present invention is preferably 0.001% by mass or more, more preferably 0.02% by mass or more. The upper limit is not particularly limited, but usually 90% by mass or less is preferable.

  In addition, components, such as (alpha)-glucosyl rutin contained in the composition or agent of this invention can be confirmed by the chromatogram of HPLC, The content of each component or the purity of a specific component is the peak area of a chromatogram It can be calculated from

  In the case of oral intake (oral administration), the effective amount of quercetin glycoside which is an active ingredient in the composition or agent of the present invention depends on the condition and age of the subject, but preferably per day per adult, for example. 10 to 2500 mg is preferable, 50 to 1000 mg is more preferable, and 100 to 500 mg is more preferable.

  The amount described above may be taken (administered) once a day, or may be taken (administered) divided into multiple times a day. As used herein, "effective amount" means an amount effective to reduce the subject's feeling of fatigue or to improve stiffness. The said significant amount can be suitably set by those skilled in the art in consideration of the description of the example of this specification, etc.

  The agent of the present invention may be directly taken (administered) as a supplement or the like, or may be used as an additive for imparting at least one of a fatigue-relieving action and a stiffness-improving action to a composition such as food and drink. Good. In the composition of the present invention, quercetin glycoside which is an active ingredient can be blended as it is or in the form of an agent containing quercetin glycoside.

  The composition of the present invention may be formulated as an additive for adding at least one of a fatigue-relieving action and a stiffness-improving action, and the composition of the present invention is not particularly limited. Pharmaceutical compositions are mentioned.

  In the present invention, food and drink are classified into cosmetic food / health food, functional indication food, food for specified health use, dietary supplement, food with indication for reduction of disease risk, food for sick people, etc. Is included. The disease risk reduction indication includes, for example, an indication that it is for reducing, improving, treating, alleviating and / or suppressing fatigue and / or stiffness.

  Specific examples of the food and drink include, for example, supplements; carbohydrate-containing food and drink such as rice, fish, noodles, bread and pasta; Western confections such as cookies and cakes; , Gums, and various confectionery products such as frozen or frozen desserts such as jelly, yogurt and pudding; juices, soft drinks, milk drinks, tea drinks, jelly drinks, powder drinks, functional drinks, nutritional supplement drinks and non-alcohol beer Various beverages such as beer; alcoholic beverages such as beer and low-malt beer; liquid food and drink such as soup, miso soup and soup; processed products using eggs; processed products of seafood or livestock meat;

  Moreover, the food-drinks in this invention can contain other components, such as a nutritional supplement component other than the said active ingredient. Such components include, for example, vitamins, minerals, various plants and their extracts, purified products and fractions, microorganisms and their growth factors and microbial products, dietary fibers and their enzymatic degradation products, animals and their substances Extracts, purified products, degradation products and products, various oligosaccharides, lipids, various proteins and protein degradation products can be mentioned.

  The pharmaceutical composition of the present invention can be formulated using a pharmaceutically acceptable carrier according to a method commonly practiced in the art.

  The composition or agent of the present invention is not particularly limited as long as the desired effects of the present invention can be obtained. For example, routes such as oral (eg, buccal, sublingual, etc.), parenteral (eg, eye drops, intravenous, intramuscular, subcutaneous, transdermal, transnasal, transpulmonary, etc.) can be mentioned. Among these, a less invasive route is preferable, and oral is more preferable.

  One embodiment of the composition or agent of the present invention for oral ingestion (oral administration) includes, for example, solid embodiments such as powder, fine granules, granules, capsules, sachets, tablets, tablets, boluses, lozenges, etc .; And liquid embodiments such as extracts, suspensions, syrups, elixirs, emulsions, dispersions, etc .; and semi-liquid, cream, paste and the like.

  The composition or agent of the present invention may be taken in the form of a pill (powder or concentrate in a capsule) or after being put in or dissolved in a liquid such as water or hot water (similar to drinking powdered tea) It may be taken (administered) in the form of powder or granules (including freeze-dried granules).

  One embodiment of the composition or agent of the present invention for parenteral administration is, for example, an eye drop or composition such as an aqueous solution, a suspension, an emulsion, a liquid such as a dispersion, etc .; semi-liquid, creamy, paste Ophthalmic solution or composition such as aqueous solution, suspension, emulsion, dispersion liquid etc. drop solution or composition; aqueous solution, suspension, emulsion, dispersion liquid etc. intravenous injection or Composition, intramuscular injection or composition or subcutaneous injection or composition; transdermal administration agent or composition such as liquid such as aqueous solution, suspension, emulsion, dispersion, etc .; aqueous solution, suspension, emulsion, dispersion Intranasal administration or composition or transpulmonary administration or composition such as body fluid etc. powder, fine granules etc. Suppository or composition such as rectal suppository or composition or vaginal suppository or composition etc. Aspect, and the like.

  The composition or agent of the present invention may be added to quercetin glycosides, and any conventional auxiliary ingredient used for producing solid dosage forms or liquid dosage forms, such as excipients, diluents, buffers. One or more of agents, flavoring agents, coloring agents, flavoring agents, binders, surfactants, thickeners, lubricants, suspending agents, preservatives, antioxidants, etc. may be contained.

  The timing at which the composition or agent of the present invention is ingested (administered) is not particularly limited. However, since the composition or agent of the present invention is effective, fatigue, neck, shoulder and waist stiffness It is preferable to take (administer) when you feel muscle fatigue and / or. In addition, it is preferable to take (administer) at a time zone (eg, the evening) in which fatigue, neck, shoulder and waist stiffness and / or muscle fatigue are easily felt (eg, in the evening) or before and after the VDT work.

  Hereinafter, the present invention will be described in detail based on examples, but the embodiments of the present invention are not limited to the examples.

Example 1
In order to evaluate the improvement effect on stiffness due to VDT work, as shown below, using a placebo-controlled double-blind comparative crossover method, a subjective index (visual evaluation scale, hereinafter abbreviated as VAS) is used for 18 men and women And objective indicators [appearing frequency of high frequency component of adjustment fine movement high frequency component 1 in the distance vision (at the time of adjustment resting), hereinafter abbreviated as HFC 1].

The experimental schedule was as follows.
9 am to 9:20: Take a break with an eye mask without looking at the PC and listen to music for the last 5 minutes of the break.
・ 9:20 am: Conducted the first VAS questionnaire.
-9: 20 am-9:30 am: 1st HFC 1 measurement.
9:30 am: Take the sample.
9:30 am to 10 am: VDT load.
・ 10 am: Conducted the second VAS questionnaire.
10:00 am to 10:10 am: The second HFC1 measurement.
10:10 am-10:30 am: Take a break with an eye mask without looking at the PC, and listen to music for the last 5 minutes of the break.
-10:30 am-10:40 am: The 3rd HFC1 measurement.

  In the VDT work, a personal computer monitor was installed at a distance of 30 cm from the eye, and alphabetic typing work was performed for 30 minutes. As samples, prepare test food (quercetin glucoside-blended hard capsule containing 187.5 mg of α-monoglucosyl rutin) and control food (quercetin glucoside-free hard capsule) and prepare each capsule at 9:30 Grain intake. The contents of the hard capsule of the test food and the control food are shown in Table 1.

  The VAS questionnaire measured the length from the left end of the 10 cm line to the hatched position for the items “neck and shoulder stiffness” and “waist stiffness” as the response value. As for the answer value, 10 is the best, 0 is the worst, and higher values mean the improvement. That is, for the items of "neck and shoulder stiffness" and "hip stiffness", "very stiff" is the worst state, and "no stiffness at all" is the best state. The results of the evaluation of the “neck and shoulder stiffness” and the “hip stiffness” by the VAS questionnaire are shown in FIGS. 1A and 1B, respectively.

  Moreover, about HFC1 measurement, the value of HFC1 using the autoref keratometer ARK-560 (made by Nidek) and eye control function analysis software AA-2 (made by Nidek) was evaluated for the tension state of the ciliary muscle. The results are shown in FIG.

  As shown in FIG. 1A and FIG. 1B, in the evaluation of subjective symptoms of neck and shoulder stiffness and waist stiffness by the VAS scale, no significant change appeared in the group receiving the control food, while the test food was The group ingested significantly improved the VAS scale after loading and after rest as compared to the group ingested the control food. From the results, it was shown that intake of quercetin glycoside reduces fatigue and / or improves stiffness.

  In addition, as shown in FIG. 2, in the assessment of ciliary muscle tone by HFC1 measurement, the group receiving the test food compared with the group receiving the control food, before and after ingestion and after rest The value of HFC1 decreased significantly. From this result, intake of quercetin glycoside relaxes the ciliary muscle and relieves tonicity, and by adjusting the sympathetic and parasympathetic nerve balance, the feeling of fatigue is reduced and / or stiffness is improved. The possibility was suggested.

  The composition or agent of the present invention has the effect of reducing fatigue and / or improving stiffness in a single dose and in a short time. From this feature, the composition or agent of the present invention is expected to be used for new food and drink, pharmaceutical composition and the like for reducing, improving, treating, treating and / or suppressing fatigue and / or stiffness. Be done.

Claims (3)

  A composition for relieving fatigue or improving stiffness comprising quercetin glycoside as an active ingredient.   The composition for relieving fatigue or improving stiffness according to claim 1, wherein the quercetin glycoside is α-glucosylrutin. The composition for relieving fatigue or for improving stiffness according to claim 2, wherein the α-glucosylrutin is α-monoglucosylrutin.

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